ADTL-EI1712 - CAS 2414916-45-1

ADTL-EI1712 is a dual inhibitor of ERK1 and ERK5 (IC50s = 40.43 and 64.5 nM, respectively) .1It reduces ERK1 and ERK5 activity by 93.5% and 89.4%, respectively, but also inhibits ERK2 activity by 92.7%, in a panel of 100 kinases at 1 μM. ADTL-EI1712 inhibits proliferation of HL-60 and MKN74, but not HeLa, cancer cells (IC50s = 1.26, 2.55, and >50 μM, respectively) . It reduces tumor growth and intratumor phosphorylation of ERK1/2 and ERK5 in an MKN74 mouse xenograft model when administered at a dose of 50 mg/kg per day.

Others, ERK

MAPK, Others

2414870

C22H18Cl2N4O2S2

505.44

C(N)(=O)C=1C2=C(SC1NC(=O)C3=C(Cl)C=CC=C3)CN(C(NC4=C(Cl)C=CC=C4)=S)CC2

-20°C

Ice Packs

Small Compound